Bright Minds Biosciences Inc. announced the successful completion of its three-part Phase 1 study of BMB-101. The study, conducted in Adelaide, Australia, by CMAX Clinical Research, a clinical trial center specializing in a range of early-phase trials and first-in-human studies, evaluated the safety, tolerability, pharmacokinetic (PK), and food effect in healthy volunteers. BMB-101 is a highly selective and potent 5-HT2C agonist being developed for the treatment of refractory epilepsies and other indications, such as psychosis, addiction, and impulse control disorders. BMB-101 demonstrated an excellent safety and tolerability profile. 5-HT2C target engagement was demonstrated by transient, dose-dependent increases in prolactin. BMB-101 exhibited predictable plasma pharmacokinetics with relatively small inter-individual variability. Compared to Lorcaserin, BMB-101 exhibits strong Gq unbiased signaling, coupled with minimal beta-arrestin recruitment. Bright Minds believes that G-protein unbiased signaling translates to better tolerance profile for this second-generation 5-HT2C agonists, making BMB-101 a best-in-class 5-HT2C agonism. Mechanistically, Serotonin (5-Hydroxytryptamine, 5-HT) is a monoamine neurotransmitter widely expressed in the central nervous system, and drugs modulating 5-HT have made a major impact in mental health disorders. Central 5-HT systems have long been associated with the control of ingestive behaviors and the modulation of the behavioral effects of psychostimulants, opioids, alcohol, and nicotine. Results of clinical trials and animal studies indicate that 5-HT2C receptor agonists may have therapeutic potential in the treatment of addiction by decreasing the intake of opioids as well as impulsive behavior that can escalate compulsive drug use. BMB-101 is an new chemical entity (NCE) and constitutes as a novel scaffold 5-HT2C agonistic. 5-HT2C agonized is a well proven anticonvulsant mechanism. In translational animal models, BMB-101 demonstrated a significant reduction in both the number and intensity of epileptic seizures and is a promising candidate for the treatment of Dravet Syndrome and other epilepsies. BMB-101, a highly selective 5-HT2C, Gq-protein biased agonist, has demonstrated compelling activity in a host of in vitro and in
vivo nonclinical tests. Compared to Lorcaserin, BMB-101 exhibits strong Gq biased signaling, coupled with minimal beta-
arrestin recruitment. Bright Minds believes that G-protein biased signaling translates to better tolerance profile for this second-
generation 5-HT2C agonist, making BMB-101 a best-in-class 5-HT2C agonist. Mechanistically, Serotonin (5-Hydroxytryptamine,
5-HT) is a monoamine neurotransmitter widely expressed in the central nervous system, and drugs modulating 5-HT have
made a major impact in mental health disorders. Central 5-HT systems have long been associated with the control of ingestive
behaviors and the modulation of the behavioral effects of psychostimulants, opioids, alcohol, and nicotine. Results of clinical
trials and animal studies indicate that 5-HT2C receptor agonists may have therapeutic potential in the treatment of addiction by
decreasing the intake of opioids as well as impulsive behavior that can escalate compulsive drug use. BMB-101 is a new
chemical entity (NCE) and constitutes as a novel scaffold 5-HT2C agonist. 5-HT2C agonism is a well proven anticonvulsant mechanism. In translational animal models, BMB-101 demonstrated a
significant reduction in both the number and intensity of epileptic seizures and is a promising candidate for the treatment of
Dravet Syndrome and other epilepsies. The Phase 1 trial (NCT 05397041) has been completed and BMB-101 is now Phase 2
ready.